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American Society for Microbiology, Antimicrobial Agents and Chemotherapy, 5(48), p. 1895-1899, 2004

DOI: 10.1128/aac.48.5.1895-1899.2004

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Inhibition of Human Immunodeficiency Virus Type 1 Tat-trans-Activation-Responsive Region Interaction by an Antiviral Quinolone Derivative

This paper is made freely available by the publisher.
This paper is made freely available by the publisher.

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Abstract

ABSTRACT WM5, a 6-aminoquinolone derivative, binds with high affinity to the bulge of the trans -activation-responsive region (TAR), whereas it displays low binding affinity for the loop and stem regions of TAR and for random RNA and DNA sequences. Furthermore, WM5 disrupts the natural protein-nucleic acid complex with a 50% inhibitory concentration in the low micromolar range in both in vitro and in vivo assays.